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Defactinib hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Defactinib hydrochloride图片
CAS NO:1073160-26-5
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
PF 04554878 hydrochloride
VS-6063 hydrochloride
产品介绍
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) 是一种新型 FAK 抑制剂,抑制 FAK 在 Tyr397 位点磷酸化,这种作用具有时间和剂量依赖性。

产品描述

Defactinib hydrochloride is a novel inhibitor of FAK. Which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

体外活性

Defactinib inhibits pFAK expression within 3 hours, with a gradual return of expression by 48 hours. Defactinib inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. RPPA data displays that Defactinib reduces levels of AKT and YB-1 in taxane-resistant cell lines. The expression of pFAK (Tyr397) is statistically significantly inhibited by Defactinib in a dose-dependent manner in all cell lines [1].

体内活性

There is an 87.4% reduction in tumor weight by PTX monotherapy in the HeyA8 model, and combination therapy resulted in the greatest tumor weight reduction, with a 97.9% reduction (P=0.05 compared with PTX). Defactinib (25 mg/kg; twice a day or greater statistically; 3 hours) treatment significantly inhibits pFAK (Tyr397), with return of expression noted by 24 hours. Therefore, administration of Defactinib at 25 mg/kg twice a day is selected as the dosing schedule for subsequent therapy experiments. For therapy experiments, female nude mice bearing HeyA8 tumors in the peritoneal cavity are randomly divided into 4 groups (n=10 per group): 1) vehicle orally twice daily and phosphate-buffered saline intraperitoneally weekly (control); 2) Defactinib 25 mg/kg orally twice daily; 3) PTX intraperitoneally weekly; and 4) both VDefactinib 25 mg/kg orally twice daily and PTX intraperitoneally weekly. In the SKOV3ip1 model, a 92.7% tumor weight reduction is observed in the combination group compared with PTX (P<0.001)[1].

Cas No.

1073160-26-5

分子式

C20H22ClF3N8O3S

分子量

546.95

别名

PF 04554878 hydrochloride;VS-6063 hydrochloride

储存和溶解度

DMSO:22.5mg/mL (41.1mM),Need ultrasonic
H2O:0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years